PNAS 2013-04-23

Protein chemical synthesis by serine and threonine ligation.

Yinfeng Zhang, Ci Xu, Hiu Yung Lam, Chi Lung Lee, Xuechen Li

Index: Proc. Natl. Acad. Sci. U. S. A. 110(17) , 6657-62, (2013)

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Abstract

An efficient method has been developed for the salicylaldehyde ester-mediated ligation of unprotected peptides at serine (Ser) or threonine (Thr) residues. The utility of this peptide ligation approach has been demonstrated through the convergent syntheses of two therapeutic peptides--ovine-corticoliberin and Forteo--and the human erythrocyte acylphosphatase protein (∼11 kDa). The requisite peptide salicylaldehyde ester precursor is prepared in an epimerization-free manner via Fmoc-solid-phase peptide synthesis.